6-Aryl-3-pyrrolidinylpyridines as mGlu5 receptor negative allosteric modulators
Graphical abstract
A series of 6-aryl-3-pyrrolidinylpyridine analogs was explored as structurally novel negative allosteric modulators of the mGlu5 receptor lacking an alkyne or oxadiazole moiety. Compounds in this series were characterized by tractable SAR, good in vitro potencies and brain penetration in rodents.
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Acknowledgements
We are grateful to Drs. Mark Hayward, Qing-Ping Han, Chi Zhang and Xu Zhang, in the CPS Department, for determinations of physicochemical properties and the resolution of compound 11g, to Christina L. Bonvicino and Xiaosui Pu for in vitro pharmacology determinations and to Dr. Albert J. Robichaud for his support during this work and for helpful comments to this manuscript.
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